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BML-190 (Indomethacin morpholinylamide) is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $39 | In Stock | |
25 mg | $64 | In Stock | |
50 mg | $97 | In Stock | |
100 mg | $172 | In Stock | |
200 mg | $285 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
Description | BML-190 (Indomethacin morpholinylamide) is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor. |
Targets&IC50 | CB2:435 nM(Ki) |
In vitro | BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 potentiates the forskolin-stimulated accumulation of cAMP. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB2 receptor. 10 μM of BML-190 decreases inositol phosphates accumulation by 38%. [1] BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products. [2] BML-190 diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. BML-190 also inhibits LPS-induced PGE2 production and COX-2 induction. [3] |
Cell Research | 293/CB2 cells are labeled with [3H]adenine (1 μCi/mL) in MEM with 1% FBS for 20 hours-24 hours. Labelled cells are challenged with 50 μM forskolin and appropriate BML-190 for 30 minutes at 37°C and assayed for cAMP accumulation. For IP assays, 2 × 105 293/CB2 cells are transiently transfected with 16z44 and/or pcDNA3 using transfection reagents. Cells are labelled, challenged with BML-190 and assayed for IP production. Triplicates are performed for each data point and at least three separate trials are done for each ligand.(Only for Reference) |
Alias | Indomethacin morpholinylamide, IMMA, BML 190 |
Molecular Weight | 426.89 |
Formula | C23H23ClN2O4 |
Cas No. | 2854-32-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 21 mg/mL (49.2 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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